2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. Navarixin

Navarixin  (Synonyms: SCH 527123; MK-7123)

Cat. No.: HY-10198 Purity: 99.33%
COA
SDS
Handling Instructions Technical Support

Navarixine (SCH 527123) est un antagoniste des CXCR1 et CXCR2 qui est puissant, allostérique et oralement actif, avec Kd valeurs de 41 nM pour cynomolgus CXCR1 et 0,20 nM, 0,20 nM, 0,08 nM pour souris, rat et cynomolgus monkey CXCR2, respectivement.

Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.

For research use only. We do not sell to patients.

CAS No. : 473727-83-2

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of Navarixin:

Navarixin Related Antibodies

Top Publications Citing Use of Products

31 Publications Citing Use of MCE Navarixin

Cell Proliferation/Viability Assay
Cell Migration/Invasion Assay
Bio/Physico-chemical Assay
Flow Cytometry
Histological Imaging/Staining

    Navarixin purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Dec 9;42(12):2015-2031.e11.  [Abstract]

    Navarixin (1 mg/200 mL; i.g.; once daily) significantly restricted the growth of PyMT-B6-ZsGreen tumors undergoing RIPK3-induced necroptosis.

    Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036.  [Abstract]

    CXCR1/2 inhibitor Navarixin (SCH 527123) (50 μM; 2 h) abrogated neutrophil migration by organoid-conditioned medium.

    Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036.  [Abstract]

    Navarixin (SCH 527123) (50 μM; 6 h) partially prevented increased expression of Il6, Tnfa, Il1b and Cxcl1 in neutrophils stimulated with organoid-conditioned medium.

    Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036.  [Abstract]

    Navarixin (SCH 527123) (50 μM; 18 h) partially prevented lower levels of L-selectin and increased expression of CD11b, CXCR4, and CCR2 in neutrophils stimulated with organoid-conditioned medium.

    Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036.  [Abstract]

    Immunofluorescence of progenitor markers in liver sections of mice fed with DDC for 3 weeks and treated with Navarixin (SCH 527123) (50 mg/kg; i.g.; once daily for 3 weeks).

    View All CXCR Isoform Specific Products:

    View All Isoforms
    CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1][2].

    IC50 & Target[1][2][3]

    125I-CXCL8-CXCR2

    0.97 nM (IC50)

    Cynomolgus CXCR2

    0.08 nM (Kd)

    Mouse CXCR2

    0.2 nM (Kd)

    Rat CXCR2

    0.2 nM (Kd)

    125I-CXCL8-CXCR1

    43 nM (IC50)

    Cynomolgus CXCR1

    41 nM (Kd)

    Cellular Effect
    Cell Line Type Value Description References
    BaF3 IC50
    2.6 nM
    Compound: 4, SCH-527123
    Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells
    Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells
    		[PMID: 17181143]
    BaF3 IC50
    36 nM
    Compound: 4, SCH-527123
    Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells
    Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells
    		[PMID: 17181143]
    Caco-2 IC50
    18.78 μM
    Compound: Navarixin
    Cytotoxicity against human Caco2 cells
    Cytotoxicity against human Caco2 cells
    		[PMID: 34536673]
    In Vitro

    Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1]. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells[2]. Navarixin (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Navarixin Related Antibodies
    In Vivo

    Navarixin (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED50=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Navarixin (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED=1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50=0.1 mg/kg) induced by intratracheal (i.t.) LPS[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    397.42

    Formula

    C21H23N3O5
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[C@H](CC)C3=CC=C(O3)C)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (125.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5162 mL 12.5811 mL 25.1623 mL
    5 mM 0.5032 mL 2.5162 mL 5.0325 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.29 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References
    Cell Assay
    [2]

    Recombinant cells are resuspended at 1×106/mL in assay buffer (phenol red free-RPMI 1640 supplemented with 2% FBS). Human neutrophils are resuspended at 2 × 106/mL in the same assay buffer containing 5% FBS. CXCL1 binds only CXCR2 with high affinity, whereas CXCL8 binds both CXCR1 and CXCR2 with high affinity. Chemoattractants (30 μL) diluted in assay buffer are dispensed into the bottom wells of disposable microchemotaxis plates, which are then covered with filter. Cells are preincubated with Navarixin (1-300 nM) in a CO2 incubator for 90 min. Cell aliquots (25 μL) are applied to each spot on the filter. After incubation (90 min for BaF/3 cells and 30 min for PMN in a CO2 incubator), the filters are removed[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Male BALB/c mice weighing between 20 and 25 g are used. Control mice receive intranasal injection of 50 μL of isotonic (0.9%) saline. Navarixin (0.1-10 mg/kg, p.o.) is suspended in 0.4% methylcellulose and given orally by gavage 2 h before and 4 h after each intranasal administration of LPS. Control animals receive 0.4% methylcellulose (10 mL/kg). In total, four doses of Navarixin or vehicle are given[1].
    Rats[1]
    Male Sprague-Dawley rats (200 g) are used. Control animals receive 100 μL of isotonic saline. Navarixin (0.1-3 mg/kg, p.o.) is suspended in 0.4% methylcellulose vehicle and given orally 2 h before the LPS challenge. Control rats receive oral methylcellulose (10 mL/kg). Only one dose of Navarixin or vehicle is given in these experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5162 mL 12.5811 mL 25.1623 mL 62.9057 mL
    5 mM 0.5032 mL 2.5162 mL 5.0325 mL 12.5811 mL
    10 mM 0.2516 mL 1.2581 mL 2.5162 mL 6.2906 mL
    15 mM 0.1677 mL 0.8387 mL 1.6775 mL 4.1937 mL
    20 mM 0.1258 mL 0.6291 mL 1.2581 mL 3.1453 mL
    25 mM 0.1006 mL 0.5032 mL 1.0065 mL 2.5162 mL
    30 mM 0.0839 mL 0.4194 mL 0.8387 mL 2.0969 mL
    40 mM 0.0629 mL 0.3145 mL 0.6291 mL 1.5726 mL
    50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2581 mL
    60 mM 0.0419 mL 0.2097 mL 0.4194 mL 1.0484 mL
    80 mM 0.0315 mL 0.1573 mL 0.3145 mL 0.7863 mL
    100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6291 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Navarixin Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Navarixin473727-83-2SCH 527123 MK-7123SCH527123SCH-527123MK7123MK 7123MK-7123CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Navarixin
    Cat. No.:
    HY-10198
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (640 KB) Français - FR (640 KB) Deutsch - DE (640 KB) Norwegian - NO (640 KB) Español - ES (640 KB) Swedish - SV (640 KB) Italian - IT (640 KB) Korean - KR (640 KB) Portuguese - PT (640 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.